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Literature summary for 2.4.1.1 extracted from

  • Onda, K.; Suzuki, T.; Shiraki, R.; Yonetoku, Y.; Negoro, K.; Momose, K.; Katayama, N.; Orita, M.; Yamaguchi, T.; Ohta, M.; Tsukamoto, S.
    Synthesis of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives as inhibitors of human liver glycogen phosphorylase a (2008), Bioorg. Med. Chem., 16, 5452-5464.
    View publication on PubMed
Search for more literature for 2.4.1.1

Crystallization (Commentary)

Crystallization (Comment) Organism
in complexwith inhibitor 5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide, inhibitor binds to a solvent cavity at the dimer interface, with the two hydroxyl groups making favorable electrostatic interactions with the enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5-chloro-N-[2-chloro-4-(1,2-dihydroxyethyl)-phenyl]-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-[4-(1,2-dihydroxyethyl)-3-(trifluoromethyl)phenyl]-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide crystallization data Homo sapiens
5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide inhibitor shows oral hypoglycemic activity in diabetic db/db mice Mus musculus
5-chloro-N-[4-(2-hydroxyethyl)phenyl]-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-[5-(1,2-dihydroxyethyl)pyrazin-2-yl]-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-[5-(1,2-dihydroxyethyl)pyridin-2-yl]-1H-indole-2-carboxamide
-
 Homo sapiens
CP-320626
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P06737 phosphorylase a
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Mus musculus
-
liver
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00025
-
 pH 6.8, 22C Homo sapiens 5-chloro-N-[5-(1,2-dihydroxyethyl)pyridin-2-yl]-1H-indole-2-carboxamide
0.00034
-
 pH 6.8, 22C Homo sapiens 5-chloro-N-[4-(1,2-dihydroxyethyl)-3-(trifluoromethyl)phenyl]-1H-indole-2-carboxamide
0.00042
-
 pH 6.8, 22C Homo sapiens 5-chloro-N-[2-chloro-4-(1,2-dihydroxyethyl)-phenyl]-1H-indole-2-carboxamide
0.00044
-
 pH 6.8, 22C Homo sapiens 5-chloro-N-[5-(1,2-dihydroxyethyl)pyrazin-2-yl]-1H-indole-2-carboxamide
0.0009
-
 pH 6.8, 22C Homo sapiens 5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide
0.00092
-
 pH 6.8, 22C Homo sapiens CP-320626
0.0012
-
 pH 6.8, 22C Homo sapiens 5-chloro-N-[4-(2-hydroxyethyl)phenyl]-1H-indole-2-carboxamide